SP141

Catalog No.S0901 Batch:S090101

Technical Data

Formula	C₂₂H₁₆N₂O
Molecular Weight	324.38	CAS No.	1253491-42-7
Solubility (25°C)*	In vitro	DMSO	65 mg/mL (200.38 mM)
		Ethanol	65 mg/mL (200.38 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

SP141 is a new class of MDM2 inhibitor that promotes MDM2 auto-ubiquitination and degradation, and reduces levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation and ability to form tumors in nude mice. SP141 inhibits human pancreatic cancer cell growth with IC50 values of less than 0.5 μM (0.38–0.50 μM) in a p53-independent manner.

Targets

MDM2 ^[1]

<0.50 μM

In vitro

SP141 can bound directly to MDM2, promoting its auto-ubiquitination and degradation by the proteasome. SP141 reduces levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation, with 50% inhibitory concentrations <0.5 μM (0.38–0.50 μM). Increasing concentrations of SP141 induces increasing levels of apoptosis and G2–M phase arrest of pancreatic cancer cell lines, whether or not they expressed functional P53.^[1]

In vivo

SP-141 (40 mg/kg; administered by i.p. injection; 5 d/wk for about three weeks) suppresses pancreatic tumor growth in both xenograft and orthotopic mouse models.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Humen pancreatic cancer cell lines Concentrations 0.01-10 μM Incubation Time 72 h Method Human pancreatic cancer cell lines (HPAC, Panc-1, AsPC-1, and Mia-Paca-2) are treated with various concentrations of SP141 or vehicle controls. And then cells are used to determine the effects of SP141 on the cell viability (MTT assay), colony formation,39 proliferation (BrdUrd incorporation assay), apoptosis, and cell cycle distribution.
Animal Study:^{^[1]}	Animal Models Nude mice bearing Panc-1 xenograft tumors Dosages 40 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
Humen pancreatic cancer cell lines
Concentrations
0.01-10 μM
Incubation Time
72 h
Method
Human pancreatic cancer cell lines (HPAC, Panc-1, AsPC-1, and Mia-Paca-2) are treated with various concentrations of SP141 or vehicle controls. And then cells are used to determine the effects of SP141 on the cell viability (MTT assay), colony formation,39 proliferation (BrdUrd incorporation assay), apoptosis, and cell cycle distribution.

Animal Study:^{^[1]}

Animal Models
Nude mice bearing Panc-1 xenograft tumors
Dosages
40 mg/kg
Administration
i.p.

References

[1] Wang W, et al. Gastroenterology. 2014 Oct;147(4):893-902.e2.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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